JP7704529B2 - インテグリン標的化リガンドとその使用 - Google Patents
インテグリン標的化リガンドとその使用 Download PDFInfo
- Publication number
- JP7704529B2 JP7704529B2 JP2020560257A JP2020560257A JP7704529B2 JP 7704529 B2 JP7704529 B2 JP 7704529B2 JP 2020560257 A JP2020560257 A JP 2020560257A JP 2020560257 A JP2020560257 A JP 2020560257A JP 7704529 B2 JP7704529 B2 JP 7704529B2
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- JP
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- Prior art keywords
- compound
- mmol
- integrin
- rnai agent
- added
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7088—Compounds having three or more nucleosides or nucleotides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/545—Heterocyclic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
- A61K47/60—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K48/00—Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
- C07K14/70546—Integrin superfamily
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
- C07K14/70546—Integrin superfamily
- C07K14/70557—Integrin beta3-subunit-containing molecules, e.g. CD41, CD51, CD61
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
- C12N15/09—Recombinant DNA-technology
- C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
- C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/10—Type of nucleic acid
- C12N2310/14—Type of nucleic acid interfering nucleic acids [NA]
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Genetics & Genomics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Zoology (AREA)
- Biotechnology (AREA)
- Biomedical Technology (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- General Engineering & Computer Science (AREA)
- Wood Science & Technology (AREA)
- Toxicology (AREA)
- Immunology (AREA)
- Gastroenterology & Hepatology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Cell Biology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Physics & Mathematics (AREA)
- Plant Pathology (AREA)
- Microbiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Peptides Or Proteins (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024232254A JP2025060958A (ja) | 2018-04-27 | 2024-12-27 | インテグリン標的化リガンドとその使用 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862663763P | 2018-04-27 | 2018-04-27 | |
| US62/663,763 | 2018-04-27 | ||
| US201962790372P | 2019-01-09 | 2019-01-09 | |
| US62/790,372 | 2019-01-09 | ||
| PCT/US2019/029393 WO2019210200A1 (en) | 2018-04-27 | 2019-04-26 | Integrin targeting ligands and uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024232254A Division JP2025060958A (ja) | 2018-04-27 | 2024-12-27 | インテグリン標的化リガンドとその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021522269A JP2021522269A (ja) | 2021-08-30 |
| JPWO2019210200A5 JPWO2019210200A5 (enExample) | 2022-06-14 |
| JP7704529B2 true JP7704529B2 (ja) | 2025-07-08 |
Family
ID=68294255
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020560257A Active JP7704529B2 (ja) | 2018-04-27 | 2019-04-26 | インテグリン標的化リガンドとその使用 |
| JP2024232254A Pending JP2025060958A (ja) | 2018-04-27 | 2024-12-27 | インテグリン標的化リガンドとその使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024232254A Pending JP2025060958A (ja) | 2018-04-27 | 2024-12-27 | インテグリン標的化リガンドとその使用 |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US20210093725A1 (enExample) |
| EP (2) | EP3784269B1 (enExample) |
| JP (2) | JP7704529B2 (enExample) |
| KR (1) | KR102787533B1 (enExample) |
| CN (2) | CN112074290B (enExample) |
| AU (1) | AU2019260738B2 (enExample) |
| BR (1) | BR112020021949A2 (enExample) |
| CA (1) | CA3097656A1 (enExample) |
| DK (1) | DK3784269T3 (enExample) |
| ES (1) | ES2983950T3 (enExample) |
| FI (1) | FI3784269T3 (enExample) |
| HR (1) | HRP20240907T1 (enExample) |
| IL (2) | IL309955A (enExample) |
| JO (1) | JOP20200266A1 (enExample) |
| MX (1) | MX2020011290A (enExample) |
| SA (1) | SA520420426B1 (enExample) |
| SG (1) | SG11202009734VA (enExample) |
| SI (1) | SI3784269T1 (enExample) |
| TW (1) | TW202014206A (enExample) |
| WO (1) | WO2019210200A1 (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113613661B (zh) | 2019-01-09 | 2025-11-14 | 箭头药业股份有限公司 | 用于抑制HIF-2α(EPAS1)的表达的RNAi试剂、其组合物和使用方法 |
| MX2023002853A (es) * | 2020-09-11 | 2023-03-31 | Arrowhead Pharmaceuticals Inc | Agentes de arni para inhibir la expresion de dux4, composiciones de dichos agentes, y metodos de uso. |
| WO2023283595A2 (en) * | 2021-07-07 | 2023-01-12 | Alnylam Pharmaceuticals, Inc. | Integrin targeting ligands for ocular delivery of rnai compounds |
| WO2024260259A1 (zh) * | 2023-06-19 | 2024-12-26 | 广东众生睿创生物科技有限公司 | 一种整合素配体及其用途 |
| WO2025252118A1 (zh) * | 2024-06-06 | 2025-12-11 | 苏州瑞博生物技术股份有限公司 | 整联蛋白αvβ6特异性配体化合物、缀合物、药物组合物及其用途 |
Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2002508355A (ja) | 1997-12-17 | 2002-03-19 | メルク エンド カムパニー インコーポレーテッド | インテグリン受容体拮抗薬 |
| JP2011519348A (ja) | 2008-03-14 | 2011-07-07 | ビセン メディカル， インコーポレイテッド | インテグリン標的化剤およびそれらを用いるｉｎｖｉｖｏおよびｉｎｖｉｔｒｏでの画像化方法 |
| JP2015506946A (ja) | 2012-01-27 | 2015-03-05 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | αＶβ３を発現する細胞への標的化送達のためのインテグリンアンタゴニスト結合体 |
| JP2016511256A (ja) | 2013-02-28 | 2016-04-14 | アローヘッド リサーチ コーポレイション | Ｅｐａｓ１関連疾患を治療するための有機組成物 |
| WO2016176532A1 (en) | 2015-04-30 | 2016-11-03 | Scifluor Life Sciences, Inc. | Tetrahydronaphthyridinyl propionic acid derivatives and uses thereof |
| WO2016196239A1 (en) | 2015-05-29 | 2016-12-08 | Arrowhead Pharmaceuticals, Inc. | Compositions and methods for inhibiting gene expression of hif2alpha |
| JP2018510139A (ja) | 2015-02-19 | 2018-04-12 | サイフルーア ライフ サイエンシズ インコーポレイテッド | フッ化テトラヒドロナフチリジニルノナン酸誘導体およびその使用法 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4522811A (en) | 1982-07-08 | 1985-06-11 | Syntex (U.S.A.) Inc. | Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides |
| US6017926A (en) * | 1997-12-17 | 2000-01-25 | Merck & Co., Inc. | Integrin receptor antagonists |
| US6048861A (en) * | 1997-12-17 | 2000-04-11 | Merck & Co., Inc. | Integrin receptor antagonists |
| US20040224986A1 (en) * | 2002-08-16 | 2004-11-11 | Bart De Corte | Piperidinyl targeting compounds that selectively bind integrins |
| EA026546B1 (ru) | 2013-01-28 | 2017-04-28 | Янссен Сайенсиз Айрлэнд Юси | Хиноксалиноны и дигидрохиноксалиноны как антивирусные средства против респираторно-синцитиального вируса |
| CN105451743B (zh) * | 2013-08-07 | 2019-11-19 | 箭头研究公司 | 用于在活体中递送RNAi触发子至肿瘤细胞的聚偶联物 |
| US11971402B2 (en) * | 2015-04-24 | 2024-04-30 | Cornell University | Methods and reagents for determination and treatment of organotropic metastasis |
-
2019
- 2019-04-26 JP JP2020560257A patent/JP7704529B2/ja active Active
- 2019-04-26 EP EP19794009.1A patent/EP3784269B1/en active Active
- 2019-04-26 ES ES19794009T patent/ES2983950T3/es active Active
- 2019-04-26 MX MX2020011290A patent/MX2020011290A/es unknown
- 2019-04-26 WO PCT/US2019/029393 patent/WO2019210200A1/en not_active Ceased
- 2019-04-26 CN CN201980028704.0A patent/CN112074290B/zh active Active
- 2019-04-26 BR BR112020021949-5A patent/BR112020021949A2/pt unknown
- 2019-04-26 HR HRP20240907TT patent/HRP20240907T1/hr unknown
- 2019-04-26 DK DK19794009.1T patent/DK3784269T3/da active
- 2019-04-26 EP EP24179088.0A patent/EP4435000A3/en active Pending
- 2019-04-26 KR KR1020207033772A patent/KR102787533B1/ko active Active
- 2019-04-26 SG SG11202009734VA patent/SG11202009734VA/en unknown
- 2019-04-26 CN CN202411099363.5A patent/CN118994152A/zh active Pending
- 2019-04-26 IL IL309955A patent/IL309955A/en unknown
- 2019-04-26 US US17/050,042 patent/US20210093725A1/en active Pending
- 2019-04-26 CA CA3097656A patent/CA3097656A1/en active Pending
- 2019-04-26 SI SI201930780T patent/SI3784269T1/sl unknown
- 2019-04-26 AU AU2019260738A patent/AU2019260738B2/en active Active
- 2019-04-26 JO JOP/2020/0266A patent/JOP20200266A1/ar unknown
- 2019-04-26 IL IL278304A patent/IL278304B2/en unknown
- 2019-04-26 FI FIEP19794009.1T patent/FI3784269T3/fi active
- 2019-04-29 TW TW108114935A patent/TW202014206A/zh unknown
-
2020
- 2020-10-27 SA SA520420426A patent/SA520420426B1/ar unknown
-
2024
- 2024-12-27 JP JP2024232254A patent/JP2025060958A/ja active Pending
Patent Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2002508355A (ja) | 1997-12-17 | 2002-03-19 | メルク エンド カムパニー インコーポレーテッド | インテグリン受容体拮抗薬 |
| JP2011519348A (ja) | 2008-03-14 | 2011-07-07 | ビセン メディカル， インコーポレイテッド | インテグリン標的化剤およびそれらを用いるｉｎｖｉｖｏおよびｉｎｖｉｔｒｏでの画像化方法 |
| JP2015506946A (ja) | 2012-01-27 | 2015-03-05 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | αＶβ３を発現する細胞への標的化送達のためのインテグリンアンタゴニスト結合体 |
| JP2016511256A (ja) | 2013-02-28 | 2016-04-14 | アローヘッド リサーチ コーポレイション | Ｅｐａｓ１関連疾患を治療するための有機組成物 |
| JP2018510139A (ja) | 2015-02-19 | 2018-04-12 | サイフルーア ライフ サイエンシズ インコーポレイテッド | フッ化テトラヒドロナフチリジニルノナン酸誘導体およびその使用法 |
| WO2016176532A1 (en) | 2015-04-30 | 2016-11-03 | Scifluor Life Sciences, Inc. | Tetrahydronaphthyridinyl propionic acid derivatives and uses thereof |
| WO2016196239A1 (en) | 2015-05-29 | 2016-12-08 | Arrowhead Pharmaceuticals, Inc. | Compositions and methods for inhibiting gene expression of hif2alpha |
Non-Patent Citations (2)
| Title |
|---|
| ACS Med. Chem. Lett.，2014年，Vol.5，pp.1207-1212 |
| J． Med. Chem.，2003年，Vol.46，pp.4790-4798 |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2019210200A1 (en) | 2019-10-31 |
| ES2983950T3 (es) | 2024-10-28 |
| JP2021522269A (ja) | 2021-08-30 |
| JP2025060958A (ja) | 2025-04-10 |
| AU2019260738B2 (en) | 2025-01-30 |
| FI3784269T3 (fi) | 2024-07-03 |
| KR102787533B1 (ko) | 2025-03-31 |
| EP3784269A1 (en) | 2021-03-03 |
| EP4435000A2 (en) | 2024-09-25 |
| KR20210005145A (ko) | 2021-01-13 |
| AU2019260738A1 (en) | 2020-10-15 |
| CN112074290A (zh) | 2020-12-11 |
| JOP20200266A1 (ar) | 2020-10-21 |
| CA3097656A1 (en) | 2019-10-31 |
| EP4435000A3 (en) | 2025-02-19 |
| CN118994152A (zh) | 2024-11-22 |
| SG11202009734VA (en) | 2020-11-27 |
| IL309955A (en) | 2024-03-01 |
| EP3784269B1 (en) | 2024-06-05 |
| IL278304B1 (en) | 2024-02-01 |
| HRP20240907T1 (hr) | 2024-10-25 |
| EP3784269A4 (en) | 2022-03-23 |
| CN112074290B (zh) | 2024-09-10 |
| IL278304B2 (en) | 2024-06-01 |
| TW202014206A (zh) | 2020-04-16 |
| IL278304A (enExample) | 2020-12-31 |
| US20210093725A1 (en) | 2021-04-01 |
| DK3784269T3 (da) | 2024-07-08 |
| MX2020011290A (es) | 2020-11-13 |
| SI3784269T1 (sl) | 2024-08-30 |
| SA520420426B1 (ar) | 2024-11-19 |
| BR112020021949A2 (pt) | 2021-01-26 |
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